A potent ATP-competitive inhibitor of ATM kinase (IC₅₀ = 13 nM; Ki = 2.2 nM); sensitizes cells to both ionizing radiation and chemotherapeutic agents; induces senescent breast, lung, and colon carcinoma cells to undergo cell death; inhibits HIV-1 replication in C8166 human T-lymophocyte…

Arachidonic acid is converted by microsomal CYP450 enzymes to a variety of epoxides, ω-1 and ω-hydroxylated compounds via what is known as the epoxidase pathway. PPOH is a selective inhibitor of the epoxygenation reactions catalyzed by specific CYP450 isozymes. PPOH inhibits the…

A potent, selective antagonist of the β2-adrenergic receptor (Ki = 0.7 nM for the β2 receptor, compared with 49.5 and 611 nM for β1 and β3 receptors, respectively); active in vivo and often used to evaluate the actions of adrenergic receptor agonists.

A potent antagonist of the type III receptor tyrosine kinases PDGFRβ, FLT3, and c-Kit (IC₅₀ = 200, 220, and 170 nM, respectively); less potently inhibits CSF-1R (IC₅₀ = 3.4 µM) and does not significantly inhibit other tyrosine or serine/threonine kinases.

An analog of folic acid and aminopterin that is used in the treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions; induces adenosine release, inhibits the metabolism of folic acid, and blocks key enzymes in the synthesis of purines and pyrimidines…

A cytotoxic, quinoline alkaloid that inhibits the DNA enzyme topoisomerase I (Top I) by binding the Top1-DNA cleavage complex and inducing DNA-strand breaks; has strong anti-tumor activity and induces DNA damage at concentrations as low as 51 nM in whole cells and 12 nM in isolated nuclei in in…

A second generation analog of amiloride that inhibits TRPP3-mediated Ca2+-activated (IC₅₀ = 0.14 μM) and ENaC (IC₅₀ = 10 nM); inhibits active sodium transport of human and ovine bronchial epithelial cells (IC₅₀s = 75 and 116 nM, respectively).

A carboxylic acid-based inhibitor of aldose reductase (IC₅₀ = 0.01-15 μM) that suppresses high glucose-induced proliferation of vascular smooth muscle cells as well as prevents high glucose-induced intracellular NADH/NAD+ increase and membrane-bound protein kinase C activation.

CAS Number: 940929-33-9 Molecular Formula: C₃₁H₃₃ClN₂O₃ • HCl Formula Weight: 553.5

An analog of latanoprost in which the hydroxyl at C-15 is inverted relative to latanoprost; binds to the FP receptor in the cat iris sphincter muscle with an IC₅₀ value of 24 µM (tested as the free acid); potential impurity in latanoprost bulk drug preparations.

A long-acting, selective β2-adrenergic agonist with bronchodilator actions (EC₅₀ = 0.25 µM) that demonstrates 2,818-fold selectivity for β2-adrenergic receptors over β1-adrenergic receptors.

A rotenoid compound with chemopreventive and chemosensitizing effects in models of skin, mammary, colon, and lung carcinogenesis; inhibits cell growth (IC50 = 8 M), blocks PI3K/Akt signaling, suppresses COX-2 expression, and induces apoptosis of premalignant and squamous HBE cells without affecting…

ML-204 selectively blocks transient receptor potential canonical 4 (TRPC4) channels (IC₅₀s = 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively). It exhibits 19-fold selectivity against TRPC6 and 9-fold selectivity against TRPC5 and does not affect TRPV1,…

A quinone which inhibits topoisomerase I at 25 μM and transglutaminase (IC₅₀ = 5 μM); reduced to β-lapachone hydroquinone by NQO1, generating ROS during its reversion to β-lapachone; sensitizes cancer cells to radiation, suppresses NF-κB activation, and drives apoptosis.

A natural triterpenoid carboxylic acid that is known to have antioxidative, antimicrobial, anti-inflammatory, and anticancer activities; inhibits Na+/K+-ATPase activity (IC50 = 24.7 μM) and blocks NF-κB activation in various human cancer cells lines (10-100 μM), inhibiting cell…

A potent inhibitor of neprilysin, a membrane metallo-endopeptidase that cleaves peptide hormones, such as enkephalins, glucagon, and bradykinin (Ki = 4-140 nM); produced in vivo via the metabolism of the prodrug acetorphan.

A form of PS that contains the abundant long-chain (16:0) palmitic acid inserted at the sn-1 and sn-2 positions; commonly used in the generation of liposomes and other types of artificial membranes.

An intermediate in the biosynthesis of NAD+ that has been used to enhance NAD biosynthesis and glucose-stimulated insulin secretion in Nampt+/- mice and high-fat diet-induced type 2 diabetes mice.

A cell-permeable, selective inhibitor of N-WASP (IC₅₀ = ~ 10 μM); directly associates with the GTPase-binding domain of N-WASP, preventing its activation by Cdc42 and PIP2; interferes with membrane transport, endocytosis, and neurological development.

An irreversible antitumor agent that induces non-apoptotic cell death selectively in tumor cells expressing the small T oncoprotein and oncogenic Ras (IC₅₀s = 1.25-5 µg/ml).

An α-glucosidase inhibitor (IC₅₀ = 5.6 µM) that delays the absorption and digestion of dietary polysaccharides by reversibly inhibiting digestive enzymes such as maltase, isomaltase, and sucrase (IC₅₀s = 0.18, 5.2, and 0.37 µM, respectively).

An inhibitor of HMG-CoA reductase (IC50 = 5 nM) that has been shown to be more effective than atorvastatin, simvastatin, or pravastatin in decreasing LDL cholesterol and increasing HDL cholesterol.

A verapamil derivative that dose-dependently blocks calcium uptake via Na+/Ca2+ exchange in diverse types of cells (Ki = 28 µM); also prevents calcium release from mitochondria induced by Ruthenium Red but not by uncouplers, respiratory inhibitors, or a chelating agent.

A blocker of KCNQ channels that potently inhibits KCNQ1 and 2 homomeric channels (IC₅₀ = 0.75 and 0.71 µM, respectively) as well as KCNQ2+3 heteromultimers (IC₅₀ = 0.6 µM); shows good in vivo potency and duration of action.

A stable, potent analog of erbstatin; inhibits EGFR tyrosine kinase in vitro with an IC50 of 0.14 µg/ml; inhibits EGF-stimulated growth in NIH3T3 cells with an IC50 value of 0.5 µg/ml; delays onset of EGF-induced DNA synthesis.

An intravenous β-lactam antibiotic that is effective against Gram-positive and Gram-negative bacteria (MICs range from 0.008-0.13 µg/ml); highly resistant to degradation by β-lactamases.

A required cofactor for many enzymes including all NOS isoforms.

A selective, ATP-competitive inhibitor of Cdk9, 2, and 7 with IC₅₀ values of 4, 38, and 62 nM, respectively; blocks the cell cycle, inhibits transcription, and induces apoptosis in multiple myeloma RPMI-8226 cells with an IC₉₀ value of 0.3 µM.

A potent ER antagonist that works by both down-regulating and degrading ERα; efficacious in the treatment of estrogen-sensitive breast cancer; fully activates ER on hippocampal neurons.

A natural macrocyclic antibiotic that inhibits RNA polymerase with selectivity for Gram-positive bacteria over Gram-negative bacteria (IC₅₀s = 0.4 and 6 μM, respectively); has potent antibacterial activity against most Gram-positive bacteria and effectively targets the Gram-positive…

A prodrug for A-771726 that regulates T lymphocyte progression through the cell cycle by selectively inhibiting de novo pyrimidine synthesis; used to slow the disease progression of rheumatoid arthritis and as an immunosuppressive agent to prevent rejection of transplant allografts and xenografts.

A selective antagonist of S1P binding to the S1P3 receptor; blocks calcium increase in HeLa cells by about 40% at 10 µM.